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DNA damage and apoptosis induction in L1210 cells by cis-diamminedichloroplatinum [II] and its new aminoflavone analogue

100%

Ciesielska E., Studzian K., Zyner E., Ochocki J., Szmigiero L.

Cellular and Molecular Biology Letters

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2000

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tom 05

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nr 4

441-450

This work compares the biological properties of cis-diammine- dichloroplatinum (cisplatin) and its new analogue cis-[Pt(AF)2Cl2] (AF stands for 3-aminoflavone), which contains two aminoflavone substituents as non-leaving ligands. Both compounds were tested for their antiproliferative activity against cultured L1210 cells, and their DNA interstrand crosslinking activity in cells and in a cell-free system. Cisplatin was found to be an approximately 6 times more cytotoxic drug than its new analogue. Platinum complexes reacted with purified calf thymus DNA in a cell-free system producing DNA interstrand crosslinks. The kinetics of crosslink formation was very similar for both compounds but the maximal level of crosslinks was 20% higher for cisplatin. In cells, however, crosslinks were produced by cisplatin, whereas this type of DNA lesion was almost undetected in cells treated with the aminoflavone analogue as assayed by DNA alkaline elution. At higher drug concentrations, strong degradation of DNA was observed in L1210 cells treated with cis- [Pt(AF)2Cl2] but not in the cells incubated with cisplatin. This DNA degradation seems to reflect very efficient apoptosis induction by cis-[Pt(AF)2Cl2] as the electrophoretic patterns of DNA from cells incubated with this drug showed a ladder typical for apoptotic cells.

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Uptake of acridinecarboxamide derivatives by L1210 cells

100%

Ciesielska E., Studzian K., Bazylak G., Pastwa E., Denny W. A., Szmigiero L.

Acta Biochimica Polonica

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1998

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tom 45

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nr 4

The uptake of six 9-aminoacridinecarboxamide derivatives by L1210 cells in relation to their lipophilicity and cytotoxic activity was studied. The amount of acridines taken up by cells was estimated by fluorimetric measurements. It was found that the uptake efficiency of this class of compounds by cells depends on the size of carboxamide residue as well as on position of the substituent. The increase of size of carboxamide chain resulted in the loss of capability of acridines to penetrate cell membrane. Cytotoxic effects of acridines were well correlated with the level of drugs accumulated by cells, whereas no clear correlation between uptake and lipophilicity was observed. It is concluded that uptake of 9-aminoacridinecarboxamides is the most important factor determining their antiproliferative activity.

3

DNA damage and apoptosis induction in L1210 cells by cis-diamminedichloroplatinum[II] and its new aminoflavone analogue

100%

Ciesielska E., Studzian K., Zyner E., Ochocki J., Szmigiero L.

Cellular and Molecular Biology Letters

|

2000

|

tom 05

|

nr 2

Ograniczanie wyników

2 Cellular and Molecular Biology Letters

1 Acta Biochimica Polonica

3 Ciesielska E.

3 Studzian K.

3 Szmigiero L.

2 Ochocki J.

2 Zyner E.

1 Bazylak G.

1 Denny W. A.

1 Pastwa E.

2 2000

1 1998

DNA damage and apoptosis induction in L1210 cells by cis-diamminedichloroplatinum [II] and its new aminoflavone analogue

Uptake of acridinecarboxamide derivatives by L1210 cells

DNA damage and apoptosis induction in L1210 cells by cis-diamminedichloroplatinum[II] and its new aminoflavone analogue